Motixafortide (BL-8040)

製品コードS9665 バッチS966501

化学情報

	Synonyms	BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₉₇H₁₄₄FN₃₃O₁₉S₂
	分子量	2159.52	CAS No.	664334-36-5
Solubility (25°C)*	体外	Water	100 mg/mL (46.3 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
in vitro	Treatment with Motixafortide (BL-8040) induces the robust mobilization of AML blasts from the BM. In addition, AML cells exposed to this compound undergo differentiation. It also induces the apoptosis of AML cells in vitro. This apoptosis is mediated by the up-regulation of miR-15a/miR-16-1, resulting in down-regulation of the target genes BCL-2, MCL-1 and cyclin-D1. Overexpression of miR-15a/miR-16-1 directly induces leukemic cell death. BL-8040-induced apoptosis is also mediated by the inhibition of survival signals via the AKT/ERK pathways.^[1]
in vivo	Motixafortide (BL-8040) induces the apoptosis of AML cells in vivo. Treatment with a BCL-2 inhibitor induces apoptosis and acts together with it to enhance cell death. This compound also synergizes with FLT3 inhibitors to induce AML cell death. Importantly, this combined treatment prolongs the survival of tumor-bearing mice and reduces minimal residual disease in vivo.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	The leukemic cell lines (MV4-11, THP-1, U937, HL-60)
	濃度	0.1 μM, 1 μM, 10 μM, 20 μM
	反応時間	24 h, 48 h
	実験の流れ	Cells are seeded in triplicate at 2×10⁵ cells/well in a total volume of 250 μl in a 96-well plate in medium supplemented with 1% FCS RPMI medium for 24hr in the presence of Motixafortide (BL-8040)/AMD3100 (0.1, 1, 10 or 20μM) or ABT-199 (0.01, 0.1, 1 or 10μM). To test the combination of this compound and ABT-199, cells are incubated for 24hr with it (20μM) and ABT-199 (0.01, 0.1, 1 or 10μM). To test the combined effects of the compound and AC220, cells are incubated for 48 hr with it (20μM), AC220 (50nM) or a combination of the two. After incubation, cells are stained with propidium iodide (PI), and the percentage of dead cells (PI+ cells) in the culture is measured using a FACSCalibur machine.
動物実験	動物モデル	female NOD scid gamma (NSG) mice (7-9 weeks old)
	投薬量	400 μg/mouse
	投与方法	SC

参考

https://pubmed.ncbi.nlm.nih.gov/28280274/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Modelling glioblastoma migration with patient-derived cells, human iPSC-derived cortical neural spheroid, and high-content imaging [ King's College London, 2023, ]	PubMed: None

Modelling glioblastoma migration with patient-derived cells, human iPSC-derived cortical neural spheroid, and high-content imaging [ King's College London, 2023, ]

PubMed: None

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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